Active substanceAmpicillin + SulbactamAmpicillin + Sulbactam
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  • Dosage form: & nbsppowder for solution for intravenous and intramuscular administration
    Composition:

    Per 1 bottle:

    Active substance

    250 mg

    500 mg

    1000 mg

    2000 mg


    + 125 mg

    + 250 mg

    + 500 mg

    + 1000 mg

    Ampicillin sodium in recalculated for ampicillin

    265,7

    531,5

    1062,9

    2125,8

    250,0

    500,0

    1000,0

    2000,0

    Sulbactam sodium in recalculated to sulbactam

    136,8

    273,6

    547,2

    1094,4

    125,0

    250,0

    500,0

    1000,0

    Description:PThe powder is white or white with a yellowish hue.
    Pharmacotherapeutic group:Antibiotic-penicillin semisynthetic + beta-lactamase inhibitor
    ATX: & nbsp

    J.01.C.R.   Combinations of penicillins (including those with beta-lactamase inhibitors)

    Pharmacodynamics:

    Ampicillin + sulbactam is a combined preparation,has a bactericidal effect against ampicillin-sensitive microorganisms, including strains producing beta-lactamases.

    Ampicillin is a semi-synthetic penicillin with a wide spectrum of activity, inhibits the synthesis of proteins of the cell wall of pathogenic microorganisms.

    Sulbactam - irreversible inhibitor of beta-lactamases; expands the spectrum of ampicillin activity against resistant strains, the resistance of which develops under the influence of beta-lactamases; does not change the activity of ampicillin against sensitive strains; by binding to certain non-bacterial proteins of bacteria, exhibits synergism when used concomitantly with beta-lactam antibiotics. Stable in aqueous solution, has independent antibacterial activity against the family Neisseriaceae and Acinetobacter spp. and is resistant to the action of most plasmid beta-lactamases.

    Ampicillin + sulbactam is active against the following microorganisms (including strains producing beta-lactamases):

    Aerobic Gram-positive bacteria: Staphylococcus aureus (producing and non-producing beta-lactamase strains), Staphylococcus epidermidis (producing and non-producing beta-lactamase strains), Staphylococcus saprophyticus (producing and non-producing beta-lactamase strains), Streptococcus pyogenes, Streptococcus pneumoniae (including strains resistant to penicillin), Streptococcus spp. groups viridans, Enterococcus faecalis, Listeria monocytogenes.

    Aerobic Gram-negative bacteria: Escherichia coli, Proteus mirabilis, Proteus vulgaris, Klebsiella spp., Neisseria gonorrhoeae (producing and non-producing beta-lactamase strains), Moraxella catarrhalis (producing and non-producing beta-lactamase strains), Morganella morganii, Haemophilus influenzae (including strains resistant to ampicillin), Providencia rettgeri, Providencia stuartii.

    Anaerobic microorganisms: Bacteroides spp., including Bacteroides fragilis, Clostridium spp. (Besides Clostridium difficile), Peptococcus spp., Peptostreptococcus spp.

    Resistant: methicillin-resistant Staphylococcus spp., Citrobacter spp, most strains Enterobacter spp., Pseudomonas aeruginosa, Mycobacterium spp., Clostridium difficile, Chlamydia pneumoniae, Mycoplasma pneumoniae.

    Pharmacokinetics:

    Maximum serum concentrations (CmOh) ampicillin and sulbactam after intravenous (iv) administration of 1.5 g and 3 g of the drug are 40-71 μg / ml and 109-150 μg / ml for ampicillin; 21-40 μg / ml and 48-88 μg / ml for the sulbactam, respectively. After intramuscular (intramuscular) injection, 1.5 g of ampicillin + sulbactam CmOh Ampicillin varies from 8 μg / ml to 37 μg / ml, CmOh sulbactam - from 6 mcg / ml to 24 mcg / ml. The degree of binding to plasma proteins is 28% for ampicillin and 38% for sulbactam.Both sulbactam and ampicillin well distributed in a variety of tissues and fluids.

    Therapeutic concentrations after IM and IV administration are created in peritoneal and pleural fluids, interstitial fluid, intestinal wall, pelvic organs, skin and subcutaneous tissue. Poor penetrate the blood-brain barrier, with inflammation of the meninges, permeability to the cerebrospinal fluid increases.

    The half-life (T1/2) of ampicillin and sulbactam averages about 1 hour. Both components of the drug are excreted mainly by the kidneys in an unchanged form. From 75% to 85% of the administered dose of ampicillin and sulbactam are excreted by the kidneys within the first 8 hours. In patients with varying degrees of renal dysfunction T1/2 components of the drug is increased, which requires correction of the dose and the mode of administration of the drug.

    Indications:

    Infectious-inflammatory diseases caused by susceptible to ampicillin + sulbactam strains of microorganisms:

    - infections of the ENT organs (including sinusitis, otitis media, tonsillitis);

    - infections of the respiratory system (acute and exacerbation of chronic bronchitis, pneumonia, lung abscess, empyema of the pleura);

    - infectious endocarditis, bacterial meningitis, sepsis;

    - uncomplicated and complicated infections of the abdominal organs (cholecystitis, cholangitis, peritonitis, abscess of the abdominal cavity);

    - urinary tract infection (acute and exacerbation of chronic pyelonephritis, pyelitis);

    - infectious and inflammatory diseases of the pelvic organs (salpingitis, salpingoophoritis, tubo-ovarian abscess, endometritis, pelvioperitonitis);

    - gonococcal infection:

    - infections of the skin and soft tissues (erysipelas, abscess, phlegmon, wound and postoperative infection);

    - infections of bones and joints.

    Prevention of postoperative complications in operations on the abdominal and pelvic organs.

    Contraindications:

    Hypersensitivity to any of the components of the drug and other beta-lactam antibiotics; infectious mononucleosis (including when there is a measles-like rash), lymphocytic leukemia.

    The safety of the use of ampicillin + sulbactam in patients with terminal stage of chronic renal failure (creatinine clearance less than 5 ml / min) has not been established.

    When using procaine, lidocaine as a solvent - hypersensitivity to local anesthetics of the amide type, severe shock,blockade of intracardiac conduction, severe heart failure.

    Carefully:

    Bronchial asthma, pollinosis and other allergic diseases, liver failure, chronic diseases of the gastrointestinal tract in history, previously suffered colitis associated with the use of antibacterial drugs, impaired renal function, and advanced age.

    Pregnancy and lactation:

    Use during pregnancy is only possible if the intended benefit to the mother exceeds the potential risk to the fetus.

    Ampicillin and sulbactam penetrate into breast milk in low concentrations. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

    Dosing and Administration:

    Intravenously (jet and drip), intramuscularly. The mode of administration depends on the severity of the infection and the chosen dose. The following are the total doses of ampicillin and sulbactam (in a 2: 1 ratio).

    In adults and children over 12 years of age and weighing more than 40 kg for treatment of infections of an average degree of gravity enter in / m or in / in on 1,5 g every 6 hours.

    In severe infections - 3 g every 6 hours.The maximum daily dose of sulbactam should not exceed 4 g, which corresponds to a daily dose of 12 g.

    Treatment should be continued for at least another 2-3 days after the disappearance of the clinical symptoms of the disease. Duration of treatment is 5-14 days, but in more severe cases it can be increased or prescribed additionally ampicillin.

    With uncomplicated gonorrhea - 1.5 g once.

    For the prevention of postoperative infection - 1,5-3 g during anesthesia, then within 24 hours after the operation in the same dose every 6-8 hours.

    In children older than 1 month and up to 12 years of age (or weighing less than 40 kg) the drug is administered at a dose of 150 mg / kg per day, which is divided into 3-4 injections. In severe infection, the dose can be increased to 300 mg / kg / day. The duration of the course of therapy should not exceed 14 days.

    In preterm infants and children of the first week of life, the daily dose of the drug is 75 mg / kg, which is divided into two injections.

    In children from 7 days to 28 days, the drug is prescribed at a dose of 150 mg / kg per day, divided into 3 intravenous infusions.

    In patients with impaired renal function, correction of the dosing regimen is performed depending on the values ​​of creatinine clearance (CK).

    Creatinine clearance, ml / min

    T 1/2, h

    Recommended mode of administration

    ≥30

    1

    1,5-3 g every 6-8 h

    15-29

    5

    1,5-3 g every 12 h

    5-14

    9

    1,5-3 g every 24 hours

    In children with kidney failure (CC less than 30 ml / min), the drug is administered in usual single doses (50-75 mg / kg), increasing the intervals between administrations, as indicated in adults.

    Preparation of solutions:

    To prepare the solution for the / m administration, sterile water for injection, 0.5% procaine solution, 0.5% lidocaine solution is used as the solvent. 4 ml of the solvent are added to the vial containing 1.5 g of the preparation.

    To prepare a solution for IV infusion into the bottle containing 1.5 g of the drug, add 12 ml of water for injection, 0.9% solution of sodium chloride. Enter slowly for 3-5 minutes.

    To prepare a solution for intravenous drip 1.5-3 g of the drug is dissolved in 15 ml of water for injection, then the resulting solution is added to 150-200 ml of a 0.9% solution of sodium chloride or 5% solution of dextrose and injected at a rate of 60 -80 drops per minute.

    Side effects:

    Allergic reactions: urticaria, skin hyperemia, skin itch, Quincke's edema, rhinitis, conjunctivitis, fever, arthralgia, anaphylactic shock, Stevens-Johnson syndrome, multiform exudative erythema, toxic epidermal necrolysis.

    From the digestive system: nausea, vomiting, decreased appetite, diarrhea, flatulence, glossitis, pseudomembranous colitis, increased activity of "hepatic" transaminases.

    On the part of the organs of hematopoiesis: hemolytic anemia, decreased hemoglobin, thrombocytopenia, eosinophilia, leukopenia, neutropenia, lymphopenia, lymphocytosis, thrombocytosis, monocytosis, false-positive Coombs test.

    From the central nervous system: drowsiness, headache.

    Laboratory indicators: azotemia, increased urea concentration in plasma blood, hypercreatininaemia, decreased serum protein, leukocyturia, cylindruria.

    Local reactions: with the / m introduction - soreness at the injection site, with the / in the introduction - phlebitis, thrombophlebitis.

    Other: malaise, chest pain, sore throat, dysuria, swelling, bleeding; with long-term treatment - candidamycosis, the development of superinfection.

    Overdose:

    Symptoms: neurological disorders up to seizures (especially in patients with impaired renal function), nausea, vomiting, diarrhea, disturbance of water-electrolyte balance (as a consequence of vomiting and diarrhea).

    Treatment: symptomatic therapy; in severe cases - hemodialysis.

    Interaction:

    When used simultaneously with indirect anticoagulants ampicillin + sulbactam potentiates their action; reduces the effectiveness of oral contraceptives, drugs, in the process of metabolism which produces paraaminobenzoic acid and ethinyl estradiol (risk of bleeding "breakthrough").

    With simultaneous use with aminoglycosides, there is a pronounced synergism of bactericidal action against gram-positive and gram-negative bacteria.

    Pharmaceutically incompatible with blood products or protein hydrolysates, aminoglycosides. When using the drug with aminoglycosides simultaneously, do not mix drugs in one syringe or one infusion system; with the / m introduction to enter into different parts of the body; when IV introduction, enter separately, observing a certain sequence with as long a time interval between administrations, or use separate intravenous catheters.

    Probenecid, allopurinol, phenylbutazone, non-steroidal anti-inflammatory drugs reduce tubular secretion of ampicillin and sulbactam and increase their half-life. Diuretics reduce the clearance of penicillins.

    Bactericidal antibiotics (including cephalosporins, cycloserine, vancomycin, rifampicin, aminoglycosides) have a synergistic effect; bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines) - antagonistic. Simultaneous use of ampicillin and allopurinol increases the risk of skin rash.

    Special instructions:

    With prolonged use of the drug, periodic monitoring of the kidneys, liver and general blood analysis is necessary.

    Before the start of therapy, a thorough anamnesis should be made about the previous allergic reactions to beta-lactam antibiotics. When developing an allergic reaction, the drug should be immediately discontinued.

    When using the drug, both in the background of taking and 2-3 weeks after the cessation of treatment, it is possible to develop diarrhea caused by Clostridium difficile (pseudomembranous colitis). In mild cases, it is sufficient to cancel the treatment and apply ion-exchange resins (colestramine, colestipol), in severe cases, compensation for loss of fluid, electrolytes and protein, the appointment of vancomycin or metronidazole.Do not use drugs that inhibit the intestinal motility.

    With the use of ampicillin + sulbactam (as well as other antibiotics), it is possible to develop superinfection, which requires the withdrawal of the drug and the appointment of appropriate treatment.

    It is possible to detect a false positive sample of Coombs, a false positive test for glucose in the urine (using the method of Benedict or Felling).

    In the treatment of patients with sepsis, the development of a bacteriolysis reaction (the Yarisch-Gerxheimer reaction) is possible.

    Effect on the ability to drive transp. cf. and fur:

    Data on the adverse effect of the drug at recommended doses on the ability to drive a vehicle or work with mechanisms are not present. However, given the likelihood of side effects from the central nervous system, caution should be exercised when engaging in potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

    Form release / dosage:Powder for the preparation of solution for intravenous and intramuscular injection, 250 mg + 125 mg, 500 mg + 250 mg, 1000 mg + 500 mg and 2000 mg + 1000 mg.
    Packaging:

    Powder for solution for intravenous and intramuscular administration: 250 mg + 125 mg, 500 mg + 250 mg, 1000 mg + 500 mg and 2000 mg + 1000 mg of the active ingredients in a clear glass vial (USP type I) with a capacity of 10 or 20 ml, sealed with a stopper of bromobutyl rubber, covered with an aluminum ring with a plastic snap-off lid.

    Solvent: water for injections (RU No. LP-002377 dated February 18, 2014) of 1.0 ml, 1.8 ml, 3.5 ml and 10.0 ml into ampoules of colorless neutral glass or from low-density polyethylene.

    For a dosage of 250 mg + 125 mg: 1 bottle with the drug and 1 ampoule of 1 ml with or without solvent, together with instructions for use in cardboard bundle.

    For a dosage of 500 mg + 250 mg: 1 bottle with the drug and 1 ampoule of 1.8 ml with or without solvent, together with instructions for use in a cardboard pack.

    For the dosage of 1000 mg + 500 mg: For 1 bottle with the drug and 1 ampoule for 3.5 ml with or without solvent, together with instructions for use in a cardboard pack.

    For the dosage of 2000 mg + 1000 mg: 1 bottle with the drug and 1 ampoule of 10.0 ml with or without solvent, together with instructions for use in a cardboard pack.

    For hospitals:

    5, 10 and 100 vials with the drug and, respectively:

    for a dosage of 250 mg + 125 mg - 5, 10 and 100 ampoules of 1.0 ml with or without solvent, together with instructions for use in an amount equal to the number of bottles, in a cardboard box;

    for a dosage of 500 mg + 250 mg: - 5, 10 and 100 ampoules of 1.8 ml with or without solvent, together with instructions for use in an amount equal to the number of bottles, in a cardboard box;

    for a dosage of 1000 mg + 500 mg: - 5, 10 and 100 ampoules of 3.5 ml with or without solvent, together with instructions for use in an amount equal to the number of bottles, in a cardboard box;

    for a dosage of 2000 mg + 1000 mg: -5, 10 and 100 ampoules of 10.0 ml with or without solvent, together with instructions for use in an amount equal to the number of bottles, in a cardboard box.

    Storage conditions:

    Store in a dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use the drug after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003997
    Date of registration:06.12.2016
    Expiration Date:06.12.2021
    The owner of the registration certificate:JODAS EKSPOIM, LLC JODAS EKSPOIM, LLC Russia
    Manufacturer: & nbsp
    Representation: & nbspJodas Expoim, Open CompanyJodas Expoim, Open Company
    Information update date: & nbsp22.08.2017
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